Calpeptin is a potent, cell-permeable inhibitor of the Ca2+-dependent protease, calpain. Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential in rat retinal ganglion cells, and thus provides functional neuroprotection. Calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3 in a feline right ventricular (RV) PO (RVPO) model, cleavage of their substrates, and cardiomyocyte programmed cell death.
Arthritis Res Ther. 2020 May 11;22(1):110.
Increased serum calpain activity is associated with HMGB1 levels in systemic sclerosis
Calpeptin purchased from AbMole
|Source||Arthritis Research & Therapy (2020 May). Figure 2. Calpeptin (Abmole Bioscience, USA)|
|Method||Calpain activity measurement|
|Incubation Time||1 h|
|Results||To further assess the relationship between serum calpain activity and HMGB1 in the pathogenesis of SSc, we evaluated whether serum calpain activity was correlated with serum HMGB1 level and found that serum calpain activity was correlated positively with HMGB1 level.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 90 mg/mL|
The protective effects and potential mechanism of Calpain inhibitor Calpeptin against focal cerebral ischemia-reperfusion injury in rats.
Peng S, et al. Mol Biol Rep. 2011 Feb;38(2):905-12. PMID: 20473717.
Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells.
Pinter M, et al. Neurosci Lett. 1994 Mar 28;170(1):91-3. PMID: 8041520.
Synthesis of a new cell penetrating calpain inhibitor (calpeptin).
Tsujinaka T, et al. Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8. PMID: 2839170.
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